1. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation GPCR/G Protein
  2. nAChR Histamine Receptor
  3. Mecamylamine

Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Mecamylamine hydrochloride) usually boasts enhanced water solubility and stability.

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CAS No. : 60-40-2

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Top Publications Citing Use of Products

    Mecamylamine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jun;45(6):1160-1174.  [Abstract]

    Injection of Mecamylamine hydrochloride (MEC) (100 μM; 300 nL) into the SNr of mice reduced both mechanical and thermal thresholds on both hind paws.

    Mecamylamine purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2024 Dec 3;14(1):146.  [Abstract]

    Mecamylamine hydrochloride (Meca) (50uM; 500 nL; i.c.) effectively decreased the power of Den-induced more DA release events in parkinsonian mice.

    Mecamylamine purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2024 Dec 3;14(1):146.  [Abstract]

    Mecamylamine hydrochloride (Meca) (3 mg/kg; i.p.) blocked the CNO-induced (5 mg/kg) increase in DA concentration in 6-OHDA-lesioned ChAT-Cre mice.

    Mecamylamine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Jul 6.

    Mecamylamine hydrochloride (MEC) (1 mg/kg i.p.) blocked nAChRs and abolished the ACh-induced spine formation in ChAT-Cre × YFP-H mice.

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    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area[1][2][5].

    IC50 & Target

    nAChR[1], histamine receptor[2]

    Cellular Effect
    Cell Line Type Value Description References
    Oocyte IC50
    1.8 3
    Compound: 5, mecamylamine
    Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
    Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
    [PMID: 9435889]
    Oocyte IC50
    1.8 3
    Compound: 5, mecamylamine
    Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
    Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
    [PMID: 9435889]
    PC-12 EC50
    0.2 3
    Compound: 5, mecamylamine
    Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
    Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
    [PMID: 9435889]
    PC-12 EC50
    0.2 3
    Compound: 5, mecamylamine
    Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
    Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
    [PMID: 9435889]
    TE-671 EC50
    30 3
    Compound: 5, mecamylamine
    Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
    Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
    [PMID: 9435889]
    TE-671 EC50
    30 3
    Compound: 5, mecamylamine
    Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
    Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
    [PMID: 9435889]
    In Vitro

    Mecamylamine (0.5-9 μM, bath administered) increases the firing frequency of identified 5-HT DRN (dorsal raphe nucleus) neurons[1].
    Mecamylamine (0.5-9 μM, bath administered) increases the glutamatergic and decreases the GABAergic input of 5-HT DRN neurons[1].
    Mecamylamine (1 mM, 5 min) blocks the histamine receptor and the histamine-induced contractions in helically cut strips of rabbit aorta[2].
    Mecamylamine (10 μM,48 h) attenuates the effect of nicotine’s action of neuroprotection[3].
    Mecamylamine (1-100 nM, 30 min) dose-dependently attenuates endothelial tube formation in HDMVECs[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[3]

    Cell Line: SCG neurons
    Concentration: 10 μM
    Incubation Time: 48 h
    Result: Reduced the nicotine-facilitated increase in ERK1/2.
    In Vivo

    Mecamylamine (subcutaneous pumps, 50 mg/kg/day, 2 days) inhibits choroidal neovascularization (CNV) in CNV mice model[4].
    Mecamylamine (intraperitoneal injection, 0.5-1 mg/kg) has antidepressant-like effects in both the TST (tail suspension test) and FST (forced swim test) in C57BL/6J mice, which are dependent on both β2 and α7 subunits[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Choroidal neovascularization (CNV) mice model[1]
    Dosage: 50 mg/kg/day, 2 days
    Administration: Subcutaneous pumps implanted beneath the skin of the back, 200 μL and mean pumping rate of 0.5 μL/h.
    Result: Suppressed the development of CNV at Bruch’s membrane rupture sites in the absence of nicotine.
    Animal Model: C57BL/6J mice[5]
    Dosage: 0.5-1 mg/kg
    Administration: Intraperitoneal injection
    Result: Had no effect in β2 knockout mice and α7 knockout mice, but decreased immobility time in wildtype littermates in the FST.
    Clinical Trial
    분자량

    167.29

    화학식

    C11H21N

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1(C)C(NC)(C)C2CCC1C2

    선적

    Room temperature in continental US; may vary elsewhere.

    보관
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    순도&문서

    Purity: ≥90.0%

    References
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    상품명:
    Mecamylamine
    Cat. No.:
    HY-B1395A
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